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SIBUTRAMINE
Name: Ngai Ka Chun (20)
Yiu Ysz Shing (31)
Introduction
• Chemical name: Sibutramine
• IUPAC name: {1-[1-(4-chloro-phenyl)-cyclobutyl]-3•
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methyl-butyl}-dimethyl-amine
Sibutramine is a neurotransmitter reuptake inhibitor.
It can reduce the reuptake of serotonin by53%,
norepinephrine by54% and dopamine by16%.
Serotonin can affect the appetite.
Nowadays, its properties are not fully discovered.
it can inhabit the uptake of serotonin; it should be an
effective antidepressant.
It is banned in 2010
Lead compound discovery
1. Since Serotonin can promote a feeling of wellbeing and happiness,
scientists therefore do researches on Serotonin.
2. In1987, Buckett, W.R., Hopcroft, R.H., Luscombe, G.P., Thomas, P.C
are the people who first discovered BTS 545 24 (Sibutramine) , a
monoamine uptake inhibitor from 4-chlorobenzyl cyanide.
3. In1995, Kelly discovered that sibutramine can decrease an obese
person’s weight. This makes it to become an anorexiant to help obese
people to lose weight.
Molecular Modification
Formulation development
Oral :Capsule
Potential in treating diseases:
1.sexual dysfunction
2.addictive disorders
3.pulmonary hypertension
4.cardiovascular disease
5.Chronic Fatigue Syndrome
6. hyperactivity disorders
7.menstrual dysfunction
8.orthostatic hypotension.
Formulation development
a number of clinically significant interactions:
1.Sibutramine and monoamine oxidase inhibitors (MAOIs,
such as selegiline)
2.Increase the risk of serotonin syndrome
3.Sibutramine and certain medications used in the
treatment of migraines—such as ergolines and triptans
4.Increase the risk for serotonin syndrome
Safety tests and human trials
Approval for marketing:
Meridia
1.a Sibutramine product
2.Produced by Abbott of America.
3.Approved by the Food and Drug Administration in
November 1997
4.For weight loss and maintenance of weight loss in
obese people, as well as in certain overweight people
with other risks for heart disease
Approval for marketing:
Side effects:
1.cardiovascular events
2.Increases the risk of heart attacks
3.Increase the risk of strokes in patients with a history of
cardiovascular disease.
4.Increase blood pressure and pulse
The End!